Improved process for preparing gabapentin

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 227/18 (2006.01) C07C 227/06 (2006.01) C07C 229/28 (2006.01)

Patent

CA 2650978

A one pot process for preparing l-(aminomethyl)-cyclohexaneacetic acid or pharmaceutically acceptable salts thereof comprises the steps of hydrolysing 1-cyanocyclohexaneacetic acid ethyl ester with a potassium, sodium or lithium hydroxide to form a salt of 1-cyanocyclohexaneacetic acid; in-situ hydrogenating the salt of 1-cyanocyclohexaneacetic acid in the presence of a catalyst to form the salt of l-(aminomethyl)-cyclohexaneacetic acid; and isolating l-(aminomethyl)-cyclohexaneacetic acid.

La présente invention concerne un procédé en récipient unique pour la préparation de l'acide l-(aminométhyl)-cyclohexane acétique ou de ses sels pharmaceutiquement acceptables. Ledit procédé comprend les étapes suivantes: hydrolyse de l'ester éthylique de l'acide 1-cyanocyclohexane acétique à l'aide d'un hydroxyde de potassium, de sodium ou de lithium pour former un sel de l'acide 1-cyanocyclohexane acétique; hydrogénation in situ du sel de l'acide 1-cyanocyclohexane acétique en présence d'un catalyseur pour former le sel de l'acide l-(aminométhyl)-cyclohexane acétique; et isolement de l'acide l-(aminométhyl)-cyclohexane acétique.

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